Vidofludimus

Catalog No.S7262 Synonyms: SC12267, 4SC-101

Vidofludimus Chemical Structure

Molecular Weight(MW): 355.36

Vidofludimus is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Phase 2.

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Biological Activity

Description Vidofludimus is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Phase 2.
Targets
Human DHODH [1]
134 nM
In vitro

Vidofludimus causes a concentration dependent inhibition of phytohemagglutinin-stimulated PBMC proliferation via the inhibition of pyrimidine de novo synthesis. [1] Vidofludimus attenuates IL-17 secretion from colonic strips by inhibition of STAT3 and NF-κB activation. [2]

In vivo In MRLlpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. [1] In Rats, Vidofludimus (60 mg/kg, p.o.) effectively reduces macroscopic and histological pathology and the numbers of CD3+ T cells. [2] In a rat model of renal transplantation, Vidofludimus (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection. [3]

Protocol

Kinase Assay:[1]
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DHODH inhibition assay:

In vitro DHODH inhibition assay mixture contains 50 μM decycloubiquinone, 100 μM dihydroorotate, and 60 μM 2,6-dichloroindophenol. The amount of enzyme is adjusted such that an average slope of approximately 0.2 AU/min will be achieved in the assay for the positive control (eg, without inhibitor). Measurements are conducted in 50 mM TrisHCl, 150 mM KCl, 0.1% Triton X-100, and pH 8.0 at 30°C in a final volume of 1 ml. The components are mixed, and the reaction is started by adding dihydroorotate. The reaction is followed spectrophotometrically by measuring the decrease in absorption at 600 nm for 2 minutes. The assay is linear in time and enzyme concentration. Inhibitory studies are conducted in a standard assay with additional variable amounts of inhibitor. For the determination of the IC50 values (concentration of inhibitor required for 50% inhibition), eight different inhibitor concentrations are applied. Each data point is recorded in triplicates on a single measurement day.
Animal Research:[1]
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  • Animal Models: MRLlpr/lpr mice
  • Formulation: Suspended in water
  • Dosages: 300 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (281.4 mM)
Ethanol 1 mg/mL warmed (2.81 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
Suspended in water
21mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 355.36
Formula

C20H18FNO4

CAS No. 717824-30-1
Storage powder
Synonyms SC12267, 4SC-101

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID